Biochem/physiol Actions

KDOAM25 is a selective inihbitor of the KDM5 family histone demethylases JARID1A, JARID1B, JARID1C and JARID1D with IC₅₀ values ﹤ 60 nM. JARID1A and JARID1B are independently overexpressed in some cancers with JARID1B (KDM5B, PLU1) also identified as a potential oncogene, a repressor of tumour repressor genes. JARID1C (KDM5C) and JARID1D (KDM5D) are located on the X- and Y-chromosomes respectively. KDOAM25′s closest off-target is JMJD2C (selectivity >400 fold). It shows no activity on other tested 2-OG family members, including FIH, NO66, MINA53 and PHD2. KDOAM25 is active in cells.